Andrea Vilchis-Juárez, Guillermina Ferro-Flores, Clara Santos-Cuevas, Enrique Morales-Avila, Blanca Ocampo-García, Lorenza Díaz-Nieto, Myrna Luna-Gutiérrez, Nallely Jiménez-Mancilla, Martha Pedraza-López, Leobardo Gómez-Oliván
Peptides based on the cyclic Arg-Gly-Asp (RGD) sequence have been designed to antagonize the function of alpha(v)beta(3) integrin, thereby inhibiting angiogenesis. The conjugation of RGD peptides to radiolabeled gold nanoparticles (AuNP) produces biocompatible and stable multimeric systems with target-specific molecular recognition. The aim of this research was to evaluate the therapeutic response of 177Lu-AuNP-RGD in athymic mice bearing alpha(v)beta(3)-integrin-positive C6 gliomas and compare it with that of 177Lu-AuNP or 177Lu-RGD...
March 2014: Journal of Biomedical Nanotechnology
Ina Israel, Dominik Richter, Jochen Stritzker, Michaela van Ooschot, Ulrike Donat, Andreas K Buck, Samuel Samnick
The α(v)β₃ integrin is highly expressed in prostate cancer (PCa), in which it is a key player in tumour invasion, angiogenesis and metastasis formation. Therefore, α(v)β₃ integrin is considered a very promising target for molecular imaging of PCa. This study tested the potential of the novel α(v)β₃ integrin affine agent [⁶⁸Ga]NOTA-RGD in comparison with the established [¹⁸F]fluoroethylcholine (FEC) and [¹⁸F]fluorodeoxyglucose (FDG) for assessing PCa using positron emission tomography (PET)...
2014: Current Cancer Drug Targets
Lei Jiang, Richard H Kimura, Xiaowei Ma, Yingfeng Tu, Zheng Miao, Bin Shen, Frederick T Chin, Hongcheng Shi, Sanjiv Sam Gambhir, Zhen Cheng
A divalent knottin containing two separate integrin binding epitopes (RGD) in the adjacent loops, 3-4A, was recently developed and reported in our previous publication. In the current study, 3-4A was radiofluorinated with a 4-nitrophenyl 2-(18)F-fluoropropinate ((18)F-NFP) group and the resulting divalent positron emission tomography (PET) probe, (18)F-FP-3-4A, was evaluated as a novel imaging probe to detect integrin αvβ3 positive tumors in living animals. Knottin 3-4A was synthesized by solid phase peptide synthesis, folded, and site-specifically conjugated with (18/19)F-NFP to produce the fluorinated peptide (18/19)F-fluoropropinate-3-4A ((18/19)F-FP-3-4A)...
November 3, 2014: Molecular Pharmaceutics
Hinrich A Wieder, Kelsey L Pomykala, Matthias R Benz, Andreas K Buck, Ken Herrmann
Musculoskeletal tumors comprise a multitude of tumor entities with different grades of malignancy, biological behavior, and therapeutic options. Positron emission tomography (PET) using the glucose analog [18F]fluorodeoxyglucose (FDG) is an established imaging modality for detection and staging of cancer, despite some shortcomings. Numerous studies have evaluated the role of PET imaging musculoskeletal tumors beyond FDG. The use of more specific novel PET radiopharmaceuticals such as the proliferation marker [18F]fluorodeoxythymidine (FLT), the bone-imaging agent [18F]sodium fluoride, amino acid tracers ([11C]methionine, [18F]fluoroethyltyrosine), or biomarkers of neoangiogenesis ([18F]galacto-RGD) can potentially provide insights into the biology of musculoskeletal tumors with focus on tumor grading, treatment monitoring, posttherapy assessment, and estimation of individual prognosis...
April 2014: Seminars in Musculoskeletal Radiology
Chenxi Wu, Xuyi Yue, Lixin Lang, Dale O Kiesewetter, Fang Li, Zhaohui Zhu, Gang Niu, Xiaoyuan Chen
AIM: (18)F-DPA-714 is a PET tracer that recognizes macrophage translocator protein (TSPO), and (18)F-Alfatide II ((18)F-AlF-NOTA-E[PEG4-c(RGDfk)]2) is specific for integrin αvβ3. This study aims to apply these two tracers for longitudinal PET imaging of muscular inflammation, and evaluate the value of (18)F-DPA-714 in differentiating inflammation from tumor. METHODS: RAW264.7 mouse macrophage cells were used for cell uptake analysis of (18)F-DPA-714. A mouse hind limb muscular inflammation model was established by intramuscular injection of turpentine oil...
2014: Theranostics
Alessandra Monaco, Vincent Zoete, Gian Carlo Alghisi, Curzio Rüegg, Olivier Michelin, John Prior, Leonardo Scapozza, Yann Seimbille
The development of RGD-based antagonist of αvβ3 integrin receptor has enhanced the interest in PET probes to image this receptor for the early detection of cancer, to monitor the disease progression and the response to therapy. In this work, a novel prosthetic group (N-(4-fluorophenyl)pent-4-ynamide or FPPA) for the (18)F-labeling of an αvβ3 selective RGD-peptide was successfully prepared. [(18)F]FPPA was obtained in three steps with a radiochemical yield of 44% (decay corrected). Conjugation to c(RGDfK(N3)) by the Cu(II) catalyzed Huisgen azido alkyne cycloaddition provided the [(18)F]FPPA-c(RGDfK) with a radiochemical yield of 29% (decay corrected), in an overall synthesis time of 140 min...
November 15, 2013: Bioorganic & Medicinal Chemistry Letters
Ying Li, Zhibo Liu, Jerome Lozada, May Q Wong, Kuo-Shyan Lin, Donald Yapp, David M Perrin
INTRODUCTION: Arylboronates afford rapid aqueous (18)F-labeling via the creation of a highly polar (18)F-aryltrifluoroborate anion ((18)F-ArBF3(-)). HYPOTHESIS: Radiosynthesis of an (18)F-ArBF3(-) can be successfully applied to a clinically relevant peptide. To test this hypothesis, we labeled dimeric-cylcoRGD, [c(RGDfK)]2E because a) it is molecularly complex and provides a challenging substrate to test the application of this technique, and b) [c(RGDfK)]2E has already been labeled via several (18)F-labeling methods which provide for a preliminary comparison...
November 2013: Nuclear Medicine and Biology
Jinxia Guo, Lixin Lang, Shuo Hu, Ning Guo, Lei Zhu, Zhongchan Sun, Ying Ma, Dale O Kiesewetter, Gang Niu, Qingguo Xie, Xiaoyuan Chen
PURPOSE: RGD peptide-based radiotracers are well established as integrin αvβ3 imaging probes to evaluate tumor angiogenesis or tissue remodeling after ischemia or infarction. In order to optimize the labeling process and pharmacokinetics of the imaging probes, we synthesized three dimeric RGD peptides with or without PEGylation and performed in vivo screening. PROCEDURES: Radiolabeling was achieved through the reaction of F-18 aluminum-fluoride complex with the cyclic chelator, 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)...
April 2014: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Zhibo Liu, Ying Li, Jerome Lozada, May Q Wong, Jennifer Greene, Kuo-Shyan Lin, Donald Yapp, David M Perrin
INTRODUCTION: Positron Emission Tomography (PET) is a rapidly expanding, cutting edge technology for preclinical evaluation, cancer diagnosis and staging, and patient management. A one-step aqueous (18)F-labeling method, which can be applied to peptides to provide functional in vivo images, has been a long-standing challenge in PET imaging. Over the past few years, we have sought a rapid and mild radiolabeling method based on the aqueous radiosynthesis of in vivo stable aryltrifluoroborate (ArBF(3)(-)) conjugates...
August 2013: Nuclear Medicine and Biology
Iina Laitinen, Johannes Notni, Karolin Pohle, Martina Rudelius, Eliane Farrell, Stephan G Nekolla, Gjermund Henriksen, Stefanie Neubauer, Horst Kessler, Hans-Jürgen Wester, Markus Schwaiger
BACKGROUND: Expression of αvβ3 integrin is increased after myocardial infarction as part of the repair process. Increased expression of αvβ3 has been shown by molecular imaging with 18F-galacto-RGD in a rat model. The 68Ga-labelled RGD compounds 68Ga-NODAGA-RGD and 68Ga-TRAP(RGD)3 have high specificity and affinity, and may therefore serve as alternatives of 18F-galacto-RGD for integrin imaging. METHODS: Left coronary artery ligation was performed in rats. After 1 week, rats were imaged with [13N]NH3, followed by 18F-galacto-RGD, 68Ga-NODAGA-RGD or 68Ga-TRAP(RGD)3 using a dedicated animal PET/CT device...
2013: EJNMMI Research
Ingrid Dijkgraaf, Samantha Y A Terry, William J McBride, David M Goldenberg, Peter Laverman, Gerben M Franssen, Wim J G Oyen, Otto C Boerman
Integrin αv β3 receptors are expressed on activated endothelial cells during neovascularization to maintain tumor growth. Many radiolabeled probes utilize the tight and specific association between the arginine-glycine-aspartatic acid (RGD) peptide and integrin αv β3 , but one main obstacle for any clinical application of these probes is the laborious multistep radiosynthesis of (18)F. In this study, the dimeric RGD peptide, E-[c(RGDfK)]2, was conjugated with NODAGA and radiolabeled with (18)F in a simple one-pot process with a radiolabeling yield of 20%, the whole process lasting only 45 min...
May 2013: Contrast Media & Molecular Imaging
Shuanglong Liu, Tzu-Pin Lin, Dan Li, Lauren Leamer, Hong Shan, Zibo Li, François P Gabbaï, Peter S Conti
Positron emission tomography (PET) is a powerful technique for imaging biological pathways in vivo, particularly those that are key targets in disease processes. In contrast, fluorescence imaging has demonstrated to be a superior method for image-guided surgery, such as tumor removal. Although the integration of PET and optical imaging could provide an attractive strategy for patient management, there is a significant shortage of established platforms/methods for PET/optical probe construction. In this study, various reaction conditions were explored to develop a simple and fast method allowing for the introduction of [(18)F]-fluoride into BODIPY dyes...
2013: Theranostics
Shuanglong Liu, Matthew Hassink, Ramajeyam Selvaraj, Li-Peng Yap, Ryan Park, Hui Wang, Xiaoyuan Chen, Joseph M Fox, Zibo Li, Peter S Conti
18F positron emission tomography (PET) has a number of attributes that make it clinically attractive, including nearly 100% positron efficiency, very high specific radioactivity, and a short half-life of ≈ 110 minutes. However, the short half-life of 18F and the poor nucleophilicity of fluoride introduce challenges for the incorporation of 18F into complex molecules. Recently, the tetrazine-trans-cyclooctene ligation was introduced as a novel 18F labeling method that proceeds with fast reaction rates without catalysis...
March 2013: Molecular Imaging
S Ke, W Wang, X Qiu, F Zhang, J T Yustein, A G Cameron, S Zhang, D Yu, C Zou, X Gao, J Lin, S Yallampalli, M Li
Breast cancer is a heterogenetic tumor at the cellular level with multiple factors and components. The inconsistent expression of molecular markers during disease progression reduces the accuracy of diagnosis and efficacy of target-specific therapy. Single target-specific imaging agents can only provide limited tumor information at one time point. In contrast, multiple target-specific imaging agents can increase the accuracy of diagnosis. The aim of this study was to demonstrate the ability of multi-agent imaging to discriminate such differences in single tumor...
March 2013: Current Molecular Medicine
Ning Guo, Lixin Lang, Weihua Li, Dale O Kiesewetter, Haokao Gao, Gang Niu, Qingguo Xie, Xiaoyuan Chen
With favorable pharmacokinetics and binding affinity for α(v)β(3) integrin, (18)F-labeled dimeric cyclic RGD peptide ([(18)F]FPPRGD2) has been intensively used as a PET imaging probe for lesion detection and therapy response monitoring. A recently introduced kit formulation method, which uses an (18)F-fluoride-aluminum complex labeled RGD tracer ([(18)F]AlF-NOTA-PRGD2), provides a strategy for simplifying the labeling procedure to facilitate clinical translation. Meanwhile, an easy-to-prepare (68)Ga-labeled NOTA-PRGD2 has also been reported to have promising properties for imaging integrin α(v)β(3)...
2012: PloS One
Antti Saraste, Iina Laitinen, Eliane Weidl, Moritz Wildgruber, Axel W Weber, Stephan G Nekolla, Gabriele Hölzlwimmer, Irene Esposito, Axel Walch, Pia Leppänen, Irina Lisinen, Peter B Luppa, Seppo Ylä-Herttuala, Hans-Jürgen Wester, Juhani Knuuti, Markus Schwaiger
BACKGROUND: Expression of α(v)β(3) integrin has been proposed as a marker for atherosclerotic lesion inflammation. We studied whether diet intervention reduces uptake of α(v)β(3) integrin-targeted positron emission tomography tracer (18)F-galacto-RGD in mouse atherosclerotic plaques. METHODS AND RESULTS: Hypercholesterolemic LDLR(-/-) ApoB(100/100) mice on high-fat diet for 4 months were randomized to further 3 months on high-fat diet (high-fat group, n = 8) or regular mouse chow (intervention group, n = 7)...
August 2012: Journal of Nuclear Cardiology
Mohan Doss, Hartmuth C Kolb, James J Zhang, Marie-José Bélanger, James B Stubbs, Michael G Stabin, Eric D Hostetler, R Katherine Alpaugh, Margaret von Mehren, Joseph C Walsh, Michael Haka, Vani P Mocharla, Jian Q Yu
UNLABELLED: 2-((2S,5R,8S,11S)-5-benzyl-8-(4-((2S,3R,4R,5R,6S)-6-((2-(4-(3-(18)F-fluoropropyl)-1H-1,2,3-triazol-1-yl)acetamido)methyl)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxamido)butyl)-11-(3-guanidinopropyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)acetic acid ((18)F-RGD-K5) has been developed as an α(v)β(3) integrin marker for PET. The purpose of this study was to determine the biodistribution and estimate the radiation dose from (18)F-RGD-K5 using whole-body PET/CT scans in monkeys and humans...
May 2012: Journal of Nuclear Medicine
Ning Guo, Lixin Lang, Haokao Gao, Gang Niu, Dale O Kiesewetter, Qingguo Xie, Xiaoyuan Chen
PURPOSE: Non-invasive PET imaging with radiolabeled RGD peptides for α(v)β(3) integrin targeting has become an important tool for tumor diagnosis and treatment monitoring in both pre-clinical and clinical studies. To better understand the molecular process and tracer pharmacokinetics, we introduced kinetic modeling in the investigation of (18)F-labeled RGD peptide monomer (18)F-FP-c(RGDyK) (denoted as (18)F-FPRGD) and dimer (18)F-FP-PEG3-E[c(RGDyK)](2) (denoted as (18)F-FPPRGD2). PROCEDURES: MDA-MB-435 tumor-bearing mice underwent 60 min dynamic PET scans following the injection of either (18)F-FPRGD or (18)F-FPPRGD2...
December 2012: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Haokao Gao, Lixin Lang, Ning Guo, Feng Cao, Qimeng Quan, Shuo Hu, Dale O Kiesewetter, Gang Niu, Xiaoyuan Chen
PURPOSE: The α(v)β(3) integrin represents a potential target for noninvasive imaging of angiogenesis. The purpose of this study was to evaluate a novel one-step labeled integrin α(v)β(3)-targeting positron emission tomography (PET) probe, (18)F-AlF-NOTA-PRGD2, for angiogenesis imaging in a myocardial infarction/reperfusion (MI/R) animal model. METHODS: Male Sprague-Dawley rats underwent 45-min transient left coronary artery occlusion followed by reperfusion...
April 2012: European Journal of Nuclear Medicine and Molecular Imaging
Lixin Lang, Weihua Li, Ning Guo, Ying Ma, Lei Zhu, Dale O Kiesewetter, Baozhong Shen, Gang Niu, Xiaoyuan Chen
[(18)F]FPPRGD2, an F-18 labeled dimeric cyclic RGDyK peptide, has favorable properties for PET imaging of angiogenesis by targeting the α(v)β(3) integrin receptor. This radiotracer has been approved by the FDA for use in clinical trials. However, the time-consuming multiple-step synthetic procedure required for its preparation may hinder the widespread usage of this tracer. The recent development of a method using an F-18 fluoride-aluminum complex to radiolabel peptides provides a strategy for simplifying the labeling procedure...
December 21, 2011: Bioconjugate Chemistry
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